Tag: M.W=150-200

An article Design, synthesis and anticervical cancer activity of new benzofuran-pyrazol-hydrazono- thiazolidin-4-one hybrids as potential EGFR inhibitors and apoptosis inducing agents WOS:000476615700014 published article about GROWTH-FACTOR RECEPTOR; MOLECULAR DOCKING; KINASE INHIBITORS; BREAST-CANCER; IN-VITRO; DERIVATIVES; ANTICANCER; DISCOVERY in [Abbas, Hebat-Allah S.] King Khalid Univ, Coll Sci, Chem Dept, Abha, Saudi Arabia; [Abbas, Hebat-Allah S.] Natl Res Ctr, Photochem Dept, Cairo 12622, Egypt; [Abd El Karim, Somaia S.] Natl Res Ctr, Dept Therapeut Chem, Cairo 12622, Egypt in 2019.0, Cited 35.0. Safety of 2,5-Dimethoxybenzaldehyde. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

This study represents the synthetic approaches of a new set of 2-(((3-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-4-yemethylene)hydrazono)-5-(aryl)thiazolidin-4-one derivatives 4-22 aiming to obtain new antiproliferative candidates against human cervix carcinoma cells (Hela) of EGFR PK inhibiting potency. The cancer cells represented promising sensitivity towards the compounds 6, 7, 11, 13, 14, 16, 17 more than or equal to that against the reference drug doxorubicin. In addition, the latter compounds were tested as EGFR protein kinase inhibitors. The results revealed that compound 14 showed more significant EGFR PK inhibitory activity than the reference drug erlotinib (IC50; 0.07, 0.08 mu M, respectively). Moreover, cell cycle analysis and apoptosis assay were performed for compound 14 proving its ability to cause G1/S phase arrest and apoptosis in Hela cancer cells, in addition to its activation of the caspases-7 and -3. In addition, derivative 14 increased the expression level of p53 and the ratio of Bax/Bcl-2 which confirmed its mode of action. Molecular docking study of 14 was performed to investigate its binding mode of interaction with EGFR PK in the active site with the aim of rationalizing its promising inhibitory activity. Accordingly, compound 14 might be considered as a promising scaffold anticervical cancer chemotherapeutic and deserves further optimization and in-depth biological studies.

Safety of 2,5-Dimethoxybenzaldehyde. Bye, fridends, I hope you can learn more about C9H10O3, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

SDS of cas: 93-02-7. Authors Gein, VL; Prudnikova, AN; Kurbatova, AA; Rudakova, IP in SPRINGER published article about in [Gein, V. L.; Prudnikova, A. N.; Kurbatova, A. A.; Rudakova, I. P.] Perm State Pharmaceut Acad, Minist Hlth Russian Federat, 2 Polevaya St, Perm 614990, Russia in 2021.0, Cited 14.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

Aseries of dihydrotetrazolo[1,5-a]pyrimidine derivatives were synthesized via a three-component reaction of benzoylacetone with aromatic aldehydes and 5-aminotetrazole monohydrate. The obtained compounds were tested for analgesic activity using the acetic acid-induced writhing test. Their acute toxicities were determined. (7-Aryl-5-methyl-4,7-dihydrotetrazolo[1,5-a]pyrimidin-6-yl)(phenyl)methanones were found to exhibit analgesic activity comparable to that of the reference drug metamizole sodium and were low-toxicity compounds. The obtained results were indicative of good prospects for further investigation of analgesic properties in this series of compounds.

Welcome to talk about 93-02-7, If you have any questions, you can contact Gein, VL; Prudnikova, AN; Kurbatova, AA; Rudakova, IP or send Email.. SDS of cas: 93-02-7

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

In 2019.0 ARCH PHARM published article about TYROSINE KINASES; DRUG DISCOVERY; ANGIOGENESIS; MECHANISMS; LIBRARIES; KNOWLEDGE; TARGETS; CANCER; ASSAY in [Abdel-Mohsen, Heba T.; El Diwani, Hoda, I] Natl Res Ctr, Dept Chem Nat & Microbial Prod, Div Pharmaceut & Drug Ind Res, El Buhouth St,POB 12622, Cairo, Egypt; [Girgis, Adel S.] Natl Res Ctr, Dept Pesticide Chem, Cairo, Egypt; [Mahmoud, Abeer E. E.; Ali, Mamdouh M.] Natl Res Ctr, Dept Biochem, Div Genet Engn & Biotechnol, Cairo, Egypt in 2019.0, Cited 43.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. Quality Control of 2,5-Dimethoxybenzaldehyde

A new series of 2,4-disubstituted-2-thiopyrimidines 6a-t, 9a, and 9b was efficiently designed and synthesized as antiangiogenic and cytotoxic agents. Compounds 6j, 6l, and 6d showed IC50 values of 1.23, 3.78, and 3.84 mu M, respectively, against the vascular endothelial growth factor receptor-2 (VEGFR-2). Most of the synthesized 2-thiouracils showed antiproliferative activity against the HepG2 cell line (hepatocellular carcinoma) in the micromolar range, for instance, 9b, 6l, 6m, 6n, and 6j displayed IC50 = 7.92, 8.35, 8.51, 9.59, and 13.06 mu M, respectively, relative to sorafenib (III; IC50 = 10.99 mu M). Also, compounds 6j, 9a, 6m, and 6s (IC50 = 15.21, 16.96, 17.68, and 18.15 mu M, respectively) are the most potent compounds against the UO-31 cell line. Further evaluation of the effect of the synthesized candidates on VEGFR-2 in the HepG2 cell line demonstrated that compounds 6j and 6l exhibit VEGFR-2 inhibitory activity of 87% and 84%, respectively, relative to sorafenib (III; 92%). In silico docking of the synthesized hits into the binding site of VEGFR-2 showed their ability to perform the main binding interactions with the key amino acids in the binding site. Studying the in silico predicted ADME (absorption, distribution, metabolism, and excretion) parameters for the synthesized thiouracils demonstrated that they have favorable pharmacokinetic and drug-likeness properties. These results demonstrate that the 2,4-disubstituted thiouracils 6 and 9 have not only favorable antiangiogenic and antiproliferative activity but also satisfy the criteria required for the development of orally bioavailable drugs. Consequently, they represent a biologically active scaffold that should be further optimized for future discovery of potential hits.

Quality Control of 2,5-Dimethoxybenzaldehyde. Bye, fridends, I hope you can learn more about C9H10O3, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article Design and synthesis of novel tranilast analogs: Docking, antiproliferative evaluation and in-silico screening of TGF beta R1 inhibitors WOS:000603572300004 published article about GEWALD REACTION; KNOEVENAGEL CONDENSATION; MOLECULAR-PROPERTIES; CATALYTIC AMOUNT; DERIVATIVES; ANTICANCER; MECHANISM; APOPTOSIS; ACID; 2-AMINOTHIOPHENES in [Ismail, Magda M. F.; El-Zahabi, Heba S. A.; Ibrahim, Rabab S.] Al Azhar Univ, Fac Pharm Girls, Dept Pharmaceut Chem, Cairo 11754, Egypt; [Mehany, Ahmed B. M.] Al Azhar Univ, Fac Sci Boys, Dept Zool, Cairo 11754, Egypt in 2020, Cited 55. Category: isothiazole. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

The discovery of the antiproliferative potential of tranilast prompted additional studies directed at understanding the mechanisms of tranilast action. Its inhibitory effect on cell proliferation depends principally on the capacity of tranilast to interfere with transforming growth factor beta (TGFOR1) signaling. This work summarizes design, synthesis and biological evaluation of sixteen novel tranilast analogs on different tumors such as PC-3, HepG-2 and MCF-7 cell lines. The in vitro cytotoxicity was evaluated using MTT assay showed that, twelve compounds out of sixteen showed higher cytotoxic activities (IC50’s 1.1-6.29 mu M), than that of the reference standard, 5-FU (IC50 7.53 mu M). The promising cytotoxic hits (4b, 7a, b and 14c-e), proved to be selective to cancer cells when their cytotoxicity’s are examined on human normal cell line (WI-38). Then they are investigated for their possible mode of action as TGFOR1 inhibitors; remarkable inhibition of TGFOR1 by these hits was observed at the range of IC50 0.087-3.276 mu M. The cell cycle analysis of the most potent TGFOR1 inhibitor, 4b revealed cell cycle arrest at G2/M phase on prostate cancer cells. Additionally, it is clearly indicated apoptosis induction at Pre-G1 phase, this is substantiated by significant increase in the expression on the tumor suppressor gene, p53 and up regulation the level of apoptosis mediator, caspase-3. In addition, in silico study was performed for validating the physicochemical and ADME properties which revealed that, all compounds are orally bioavailable with no side effects complying with Lipinski rule. The proposed mode of action can be further explored on the light of molecular modeling simulation of the most potent compounds, 4b and 14e which were docked into the active sites of TGFOR1 to predict their affinities toward the receptor.

Category: isothiazole. Bye, fridends, I hope you can learn more about C9H10O3, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

HPLC of Formula: C9H10O3. I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Synthesis and Investigation of Tetrahydro-beta-carboline Derivatives as Inhibitors of Plant Pathogenic Fungi published in 2021.0, Reprint Addresses Phutdhawong, WS (corresponding author), Silpakorn Univ, Fac Sci, Dept Chem, Nakhon Pathom 73000, Thailand.. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde.

A series of tetrahydro-ss-carbolines substituted with an alkyl or acyl side chain was synthesized and screened for its antifungal activity against plant pathogenic fungi (Bipolaris oryzae, Curvularia lunata, Fusarium semitectum, and Fusarium fujikuroi). The structure activity relationship revealed that the substituent at the piperidine nitrogen plays an important role for increasing antifungal activities. In this series, 2-octyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (3g) displayed potent antifungal activities with a minimum inhibitory concentration of 0.1 mu g/mL, including good inhibitory activity to the radial growth of fungus at a concentration of 100 mu g/mL compared to amphotericin B.

HPLC of Formula: C9H10O3. Welcome to talk about 93-02-7, If you have any questions, you can contact Buaban, K; Phutdhawong, W; Taechowisan, T; Phutdhawong, WS or send Email.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Recommanded Product: 2,5-Dimethoxybenzaldehyde. Recently I am researching about BIOLOGICAL EVALUATION; EFFICIENT APPROACH; 3+2 CYCLOADDITION; DERIVATIVES; CYCLIZATION; INHIBITORS; NAPHTHYLAMINES; CONSTRUCTION; ANNULATION; NITRILES, Saw an article supported by the UGC, New DelhiUniversity Grants Commission, India; CSIR, New DelhiCouncil of Scientific & Industrial Research (CSIR) – India; CSIR-IICB. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Jash, M; De, S; Pramanik, S; Chowdhury, C. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde

An efficient palladium(II)-catalyzed cascade reaction of ene-yne substrates carrying cyano/aldehyde group is described. It involves successive hetero- and benz-annulations in one pot via transoxo/aminopalladation onto alkyne, followed by 1,2-addition to cyano/aldehyde, providing a convenient synthesis of both naphtho[1,2b]-furans and benzo[g]indoles. The reaction constitutes a fast intramolecular assembly through several carbon-carbon and carbon-heteroatom bond formations taking place in one pot. The reactions are operationally simple, compatible with a range of functional groups and atom-economical in nature.

Recommanded Product: 2,5-Dimethoxybenzaldehyde. Bye, fridends, I hope you can learn more about C9H10O3, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Authors Bhaskaruni, SVHS; Maddila, S; van Zyl, WE; Jonnalagadda, SB in SPRINGER published article about ONE-POT SYNTHESIS; HETEROGENEOUS CATALYST; POLYHYDROQUINOLINE DERIVATIVES; MULTICOMPONENT SYNTHESIS; EFFICIENT CATALYST; IONIC LIQUID; ACID; NANOPARTICLES; OXIDATION; ZIRCONIA in [Bhaskaruni, Sandeep V. H. S.; Maddila, Suresh; van Zyl, Werner E.; Jonnalagadda, Sreekantha B.] Univ KwaZulu Natal, Sch Chem & Phys, Westville Campus,Chiltern Hills, ZA-4000 Durban, South Africa in 2019.0, Cited 45.0. Application In Synthesis of 2,5-Dimethoxybenzaldehyde. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

An efficient protocol to synthesize a series of new 1,4-dihydropyridine derivatives under mild conditions is developed. The catalyst consists of iron loaded on zirconia (Fe2O3/ZrO2) and is reusable for up to six cycles. Excellent yields (92-98%) were obtained under room-temperature conditions in a short time (similar to 20 min) with ethanol as solvent. Different wt% of catalyst material was prepared by simple wet-impregnation technique, and materials were characterised by powder-XRD, TEM, SEM, BET and FT-IR techniques. The structures of the new 1,4-dihydropyridine derivatives were confirmed employing various spectroscopic techniques. Facile preparation and avoidance of any column separation are the main advantages of this protocol. [GRAPHICS] .

Application In Synthesis of 2,5-Dimethoxybenzaldehyde. Bye, fridends, I hope you can learn more about C9H10O3, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article Synthesis of Acyl Phosphoramidates Employing a Modified Staudinger Reaction WOS:000643163800039 published article about INHIBITORS; ALDEHYDES; ACIDS in [Currie, Iain; Sleebs, Brad E.] Walter & Eliza Hall Inst Med Res, Parkville, Vic 3052, Australia; [Currie, Iain; Sleebs, Brad E.] Univ Melbourne, Dept Med Biol, Parkville, Vic 3010, Australia in 2021, Cited 24. Category: isothiazole. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2

A one-step synthesis of acyl phosphoramidates from a variety of functionalized acyl azides has been developed employing trimethylsilyl chloride as an activating agent in a modified Staudinger reaction. The methodology was further adapted to include the in situ generation of the acyl azides from a diverse selection of carboxylic acids and hydrazide starting synthons. The reaction scope was extended to include the synthesis of imidodiphosphates and the natural product Microcin C.

Category: isothiazole. Bye, fridends, I hope you can learn more about C7H4F2O2, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Authors Marques, BC; Santos, MB; Anselmo, DB; Monteiro, DA; Gomes, E; Saiki, MFC; Rahal, P; Rosalen, PL; Sardi, JCO; Regasini, LO in BENTHAM SCIENCE PUBL LTD published article about CHALCONE DERIVATIVES; BIOLOGICAL-ACTIVITIES; MOLECULAR-PROPERTIES; LICOCHALCONE; PREDICTION; DISCOVERY; GROWTH; SERIES; AGENTS in [Marques, Beatriz C.; Santos, Mariana B.; Anselmo, Daiane B.; Regasini, Luis O.] Sao Paulo State Univ Unesp, Inst Biosci Humanities & Exact Sci, Dept Chem & Environm Sci, BR-15054000 Sao Jose Do Rio Preto, SP, Brazil; [Monteiro, Diego A.; Gomes, Eleni; Saiki, Marilia F. C.; Rahal, Paula] Sao Paulo State Univ Unesp, Inst Biosci Humanities & Exact Sci, Dept Biol, BR-15054000 Sao Jose Do Rio Preto, SP, Brazil; [Rosalen, Pedro L.; Sardi, Janaina C. O.] Univ Campinas Unicamp, Piracicaba Dent Sch, Dept Physiol Sci, BR-13083970 Piracicaba, SP, Brazil in 2020.0, Cited 43.0. Formula: C9H10O3. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

Background: Chalcones substituted by methoxyl groups have presented a broad spectrum of bioactivities, including antifungal, antibacterial and antiproliferative effects. However, a clear and unambiguous investigation about the relevance of this substituent on the chalcone framework has not been described. Objective: The purpose of this work is to assess the antibacterial, antifungal and antiproliferative activities of the two series of seventeen synthesized regioisomeric methoxychalcones. Series I and II were constituted by cbalcones substituted by methoxyl groups on rings A (5-12) and B (13-21), respectively. In addition, the library of methoxychalcones was submitted to in silico drug-likeness and pharmacokinetics properties predictions. Methods: Methoxychalcones were synthesized and their structures were confirmed by NMR spectral data analyses. Evaluations of antimicrobial activity were performed against five species of Candida, two Gram-negative and five Gram-positive species. For antiproliferative activity, methoxychalcones were evaluated against four human tumorigenic cell lines, as well as human non-tumorigenic keratinocytes. Drug-likeness and pharmacokinetics properties were predicted using Molinspiration and PreADMET toolkits. Results: In general, chalcones of series I are the most potent antifungal, antibacterial and antiproliferative agents. 3′, 4′, 5′-Trimethoxychalcone (12) demonstrated potent antifungal activity against Candida krusei (MIC = 3.9 mu g/mL), eight times more potent than fluconazole (reference antifungal drug). 3′-Methoxychalcone (6) displayed anti-Pseudomonas activity (MIC = 7.8 mu g/mL). 2′,5′-Dimethoxychalcone (9) displayed potent antiproliferative effect against C-33A (cervix), A-431 (skin) and MCF-7 (breast), with IC50 values ranging from 7.7 to 9.2 mu M. Its potency was superior to curcumin (reference antiproliferative compound), which exhibited IC50 values ranging from 10.4 to 19.0 mu M. Conclusion: Our studies corroborated the relevance of methoxychalcones as antifungal, antibacterial and antiproliferative agents. In addition, we elucidated influence of the position and number of methoxyl groups toward bioactivity. In silico predictions indicated good drug-likeness and pharmacokinetics properties to the library of methoxychalcones.

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Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Recently I am researching about COLLOID TRANSPORT; SILVER NANOPARTICLES; ANAEROBIC BIOREMEDIATION; MINERALIZATION PATHWAYS; FLOW CONDITIONS; ORGANIC-MATTER; POROUS-MEDIA; HEAVY-METALS; MOBILIZATION; TRANSFORMATION, Saw an article supported by the United States Strategic Environmental Research and Development Program (SERDP) [ER-2130]; China Scholarship CouncilChina Scholarship Council. Published in PERGAMON-ELSEVIER SCIENCE LTD in OXFORD ,Authors: Liang, XL; Radosevich, M; Loffler, F; Schaeffer, SM; Zhuang, J. The CAS is 385-00-2. Through research, I have a further understanding and discovery of 2,6-Difluorobenzoic acid. Quality Control of 2,6-Difluorobenzoic acid

In subsurface bioremediation, electron donor addition promotes microbial Fe(lII)-oxide mineral reduction that could change soil pore structure, release colloids, and alter soil surface properties. These processes in turn may impact bioremediation rates and the ultimate fate of contaminants. Columns packed with water-stable, Fe-oxide-rich soil aggregates were infused with acetate-containing artificial groundwater and operated for 20 d or 60 d inside an anoxic chamber. Soluble Fe(II) and soil colloids were detected in the effluent within one week after initiation of the acetate addition, demonstrating Fe(III)-bioreduction and colloid formation. Diffusible Br-, less diffusible 2,6-difluorobenzoate (DFBA), and non-diffusible silica-shelled silver nanoparticles (SSSNP) were used as tracers in transport experiments before and after the bioreduction. The transport of Br- was not influenced by the bioreduction. DFBA showed earlier breakthrough and less tailing after the bioreduction, suggesting alterations in flow paths and soil surface chemistry during the 20-d bioreduction treatment. Similarly, the bioreduction increased the transport of SSSNP very significantly, with mass recovery increasing from 1.7% to 25.1%. Unexpectedly, the SSSNP was completely retained in the columns when the acetate injection was extended from 20 to 60 d, while the mass recovery of DFBA decreased from 89.1% to 84.1% and Br showed no change. The large change in the transport of SSSNP was attributed to soil aggregate breakdown and colloid release (causing mechanical straining of SSSNP) and the exposure of iron oxide surfaces previously unavailable within aggregate interiors (facilitating attachment of SSSNP). These results suggest a time dependent fashion of microbial effect on the transport of diffusivity-varying tracers. (C) 2018 Elsevier Ltd. All rights reserved.

Welcome to talk about 385-00-2, If you have any questions, you can contact Liang, XL; Radosevich, M; Loffler, F; Schaeffer, SM; Zhuang, J or send Email.. Quality Control of 2,6-Difluorobenzoic acid

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com