title

طراحی، سنتز و ارزیابی بیولوژیکی فعالیتهای سمیت سلولی، ضد یکروب و ضد HIV-1 مشتقات جدید 4،3،2،1-تتراهیدروپیریمیدین

رزاقی اصل, نیما and کامرانی مقدم, مهسا and فرهنگی, بهزاد and وهاب پور, روح اله and ذبیح الهی, رضوان and سپهری, ساقی (1397) طراحی، سنتز و ارزیابی بیولوژیکی فعالیتهای سمیت سلولی، ضد یکروب و ضد HIV-1 مشتقات جدید 4،3،2،1-تتراهیدروپیریمیدین. Research in Pharmaceutical Sciences ــ 14 (2). pp. 155-166. شاپا 1735-5362

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Title

Design, synthesis and evaluation of cytotoxic, antimicrobial, and anti-HIV-1 activities of new 1,2,3,4-tetrahydropyrimidine derivatives

English Abstract

A series of new 1,2,3,4-tetrahydropyrimidine (THPM) derivatives were designed and synthesized within a one-pot three component Biginelli reaction. The structures of compounds were characterized by FT-IR, 1H-NMR, mass spectroscopy, and elemental analysis. All synthesized derivatives were screened for their cytotoxic, antimicrobial, and anti-HIV activities. Due to significant cytotoxic and antimicrobial effects of 1,2,3,4-THPM scaffold, in this study, cytotoxic and antimicrobial activities of synthesized derivatives were evaluated on two cell lines and four bacterial strains. Compounds 4e and 4k showed highest cytotoxic activity against HeLa and MCF-7 cell lines. In addition, 4c and 4d were most active against MCF-7 and HeLa cell lines, respectively. Among the compounds, 4e revealed high antimicrobial activity against four strains. According to the results, 4e possessing m-bromophenyl group at C-4 position of THPM exhibited the highest cytotoxic and antimicrobial effects. Also, all the newly synthesized compounds were evaluated for their anti-HIV-1 assay. Compounds 4l and 4a indicated remarkable anti-HIV-1 activity. It is concluded from cytotoxic, antimicrobial, and anti-HIV-1 activities that the 1,2,3,4-tertahydropyrimidines may serve as hit compounds for development of new anticancer small-molecules.

Item Type:Article
زبان سند : انگلیسی
نویسنده اول :نیما رزاقی اصل
نویسنده :مهسا کامرانی مقدم
نویسنده :بهزاد فرهنگی
نویسنده :روح اله وهاب پور
نویسنده :رضوان ذبیح الهی
نویسنده مسئول :ساقی سپهری
Additional Information:Indexed in: ESCI, Pubmed/PMC, Scopus, Embase, Google Scholar, Index Copernicus, ISC, SID, Magiran
کلیدواژه ها (انگلیسی):Anti-HIV; Antimicrobial; Biginelli; Neoplasm;1,2,3,4-Tetrahydropyrimidine.
Subjects:QV pharmacology > QV 744 Medicinal Chemistry
Divisions:School of Pharmacy > Department of Medicinal Chemistry
ID Code:11593
Deposited By: ساقی سپهری
Deposited On:21 Dec 1397 09:37
Last Modified:10 Apr 1398 11:40

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