Category: 93-02-7

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.

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Reference:
Isothiazole – Wikipedia,
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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.

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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.

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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.

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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.

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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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I found the field of Pharmacology & Pharmacy; Toxicology very interesting. Saw the article Two immunoassays for the detection of 2C-B and related hallucinogenic phenethylamines published in 2019.0. Category: isothiazole, Reprint Addresses Kuchar, M (corresponding author), Univ Chem & Technol Prague, Tech 3, Prague 16628 6, Dejvice, Czech Republic.. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde

Introduction: The use of new psychoactive substances as drugs of abuse has dramatically increased over the last years. Hallucinogenic phenethylamines gained particular popularity as they have both stimulating and psychedelic effects. Although generally perceived as safe, these illicit drugs pose a serious health risk; they have been linked to cases of severe poisoning or even deaths. Therefore, simple, cost-effective and reliable methods are needed for rapid determination of abused hallucinogens. Methods: For this purpose, two haptens derived from 2C-H were designed, synthesized and subsequently attached to a carrier protein. Polyclonal antibodies obtained from a rabbit immunized with one of the prepared immunogens were used for the development of two immunoassays. Results: In this study, a lateral flow immunoassay (LFIA) and an enzyme linked immunosorbent assay (ELISA) for the detection of 2C-B and related hallucinogenic phenethylamines in urine were developed. The presented LFIA is primarily suitable for on-site monitoring as it is simple and can provide a visual evidence of 2C-B presence within a few minutes. Its reasonable sensitivity (LODLFIA= 15 +/- 7 ng mL(-1)) allows detection of the drug presence in urine after acute exposure. For greater accuracy, highly sensitive ELISA (LODELISA= 6 +/- 3 pg mL(-1)) is proposed for toxicological quantitative analyses of positive samples captured by the LFIA. Discussion: The comparison of the ELISA with the well-established UHPLC-MS-MS method shows excellent agreement of results, which confirms good potential of the ELISA to be used for routine analyses of 2C-B and related hallucinogenic phenethylamines of both main sub-families.

Category: isothiazole. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Sulakova, A; Fojtikova, L; Holubova, B; Bartova, K; Lapcik, O; Kuchar, M or concate me.

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An article An Atom-Economic Efficient Synthesis of 1-Amidoalkyl-2-Naphthols Mediated By Hexachlorocyclotriphosphazene (HCCP) as a Novel Catalyst WOS:000483301600008 published article about ONE-POT PREPARATION; REUSABLE CATALYST; RECYCLABLE NANOCATALYST; CHEMISTRY; ACID in [Singh, Rajesh K.; Chaudhary, Shallu; Prasad, D. N.] Shivalik Coll Pharm, Dept Pharmaceut Chem, Nangal 140126, Punjab, India; [Kumar, Sahil] GD Goenka Univ, Sch Med & Allied Sci, Dept Pharm, Sohna 122103, Haryana, India in 2019.0, Cited 25.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. SDS of cas: 93-02-7

A multicomponent one-pot atom-economic reaction is performed for an efficient synthesis of 1-amidoalkyl-2-naphthol from aromatic aldehydes, beta-naphthol and amide/urea promoted by hexachlorocyclotriphosphazene (HCCP). Various techniques such as stirring, microwave irradiation and thermal technique (hot plate and oil bath) were used in different solvents for the synthesis of 1-amidoalkyl-2-naphthol derivatives with moderate to excellent yield. Among the four methods, microwave irradiation and oil bath heating provide high yield as compared to the hot plate heating and stirring method. The low yield may be due to the formation of undesired side-products due to non-uniform heating.

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An article Discovery of 4-(2-(dimethylamino)ethoxy)benzohydrazide derivatives as prospective microtubule affinity regulating kinase 4 inhibitors WOS:000541906600037 published article about BIOLOGICAL EVALUATION; POTENTIAL INHIBITORS; PROTEIN-KINASES; MARK4; CANCER; PROLIFERATION; HALLMARKS; MIGRATION; DOCKING; COMPLEX in [Khan, Nashrah Sharif; Husain, Mohammad] Jamia Millia Islamia, Dept Biotechnol, New Delhi 110025, India; [Khan, Parvez; Ahmad, Kamal; Yousuf, Mohd; Islam, Asimul; Ali, Sher; Hassan, Md Imtaiyaz] Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India; [Inam, Afreen; Azam, Amir] Jamia Millia Islamia, Dept Chem, New Delhi 110025, India in 2020.0, Cited 47.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. Application In Synthesis of 2,5-Dimethoxybenzaldehyde

Microtubule affinity regulating kinase 4 (MARK4) is a Ser/Thr kinase, considered as a potential drug target for cancer, diabetes and neurodegenerative diseases. Due to its significant role in the development and progression of cancer, different in-house libraries of synthesized small molecules were screened to identify potential MARK4 inhibitors. A small library of hydrazone compounds showed a considerable binding affinity to MARK4. The selected compounds were further scrutinized using an enzyme inhibition assay and finally two hydrazone derivatives (H4 and H19) were selected that show excellent inhibition (nM range). These compounds have a strong binding affinity for MARK4 and moderate binding with human serum albumin. Anticancer studies were performed on MCF-7 and A549 cells, suggesting H4 and H19 selectively inhibit the growth of cancer cells. The IC50 value of compound H4 and H19 was found to be 27.39 mu M and 34.37 mu M for MCF-7 cells, while for A549 cells it was 45.24 mu M and 61.50 mu M, respectively. These compounds inhibited the colonogenic potential of cancer cells and induced apoptosis. Overall findings reflect that hydrazones/hydrazone derivatives could be exploited as potential lead molecules for developing effective anticancer therapies via targeting MARK4.

Welcome to talk about 93-02-7, If you have any questions, you can contact Khan, NS; Khan, P; Inam, A; Ahmad, K; Yousuf, M; Islam, A; Ali, S; Azam, A; Husain, M; Hassan, MI or send Email.. Application In Synthesis of 2,5-Dimethoxybenzaldehyde

Reference:
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Name: 2,5-Dimethoxybenzaldehyde. In 2019.0 BIOORG CHEM published article about PNEUMOCYSTIS-CARINII; METHOTREXATE; POTENT; DERIVATIVES; PIRITREXIM; SERIES; AGENTS in [Abdelaziz, Ola A.; El Husseiny, Walaa M.; Selim, Khalid B.; Eisa, Hassan M.] Mansoura Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Mansoura 35516, Egypt in 2019.0, Cited 46.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7.

A new series of pyrido[2,3-d] pyrimidines 3-18 bearing substitution at C-5 position was synthesized. All compounds were tested for their in vitro antitumor activity against five human cancer cell lines namely; hepatocellular carcinoma (HePG2), breast carcinoma (MCF-7), human prostate carcinoma (PC3), colorectal carcinoma (HCT-116), and cervical carcinoma (Hela) using doxorubicin as a positive control. Compounds 3, 4, 9, 11, 13, 14, 15 and 17 exhibited the highest antitumor activity against the tested cell lines and were selected to screen their enzymatic inhibition against dihydrofolate reductase enzyme (DHFR) compared with the reference drug methotrexate (MTX), to explain the probable mechanism of action of the observed anticancer activity. Compound 11 displayed the highest inhibitory activity (IC50 = 6.5 mu M) among the tested compounds in comparison with MTX (IC50 = 5.57 mu M). Also, compounds 13 and 14 showed high inhibitory activity against DHFR with IC50 values 7.1 and 8.7 mu M, respectively. Comparative molecular modeling study was performed between DHFR inhibitors 11, 13 and 14 of the highest activity and 10 of the lowest activity among the eight inhibitors against MTX. Docking studies into the active site of DHFR domain showed good agreement with the obtained biological results. Finally, compound 11 was found to be best antitumor, DHFR inhibitor, and it induced the process of apoptosis at Pre-G phase and cell cycle arrest at G2/M phase in MCF-7 cells.

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