DESIGN, SYNTHESIS AND CYTOTOXICITY EVALUATION OF NEW 2-ARYL-5, 6-DIHYDROPYRROLO [2, 1-A]ISOQUINOLINE DERIVATIVES AS TOPOISOMERASE INHIBITORS

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KAKHKI SAMANEH; SHAHOSSEINI SORAYYA; ZARGHI AFSHIN

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Journal Paper

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Journal: Iranian Journal of Pharmaceutical Research Year:2014 | Volume:13 | Issue:SUPPL Page(s): 71-77

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Title

DESIGN, SYNTHESIS AND CYTOTOXICITY EVALUATION OF NEW 2-ARYL-5, 6-DIHYDROPYRROLO [2, 1-A]ISOQUINOLINE DERIVATIVES AS TOPOISOMERASE INHIBITORS

Author(s)

KAKHKI SAMANEH | SHAHOSSEINI SORAYYA | ZARGHI AFSHIN | Issue Writer Certificate

Keywords

PYRROLO [2

1-A] ISOQUINOLINES

TOPOISOMERASE INHIBITORS

MOLECULAR MODELING

CYTOTOXICITY

Abstract

Two set of 2-aryl-5, 6-dihydropyrrolo [2, 1-a] isoquinolines were designed and synthesized to evaluate their biological activities as topoisomerase inhibitors. Cytotoxic activity of the synthesized compounds 4a-e and 7a-d was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HepG2 (liver hepatocellular cells), A549 (adenocarcinomic human alveolar basal epithelial cells), T47D (Human ductal breast epithelial tumor cell line) and Hela (Human cervix cancer). According to our results, HepG2 seems to be the most sensitive cell line for these compounds with mean IC50 values ranging from 4.25 to 70.05 mM. Our results indicated that compound 7b exhibited the best potency against the tested cell lines. These results also suggest that pyrroloisoquinoline moiety constitutes a suitable scaffold to design new anti-proliferative agents.

Cites

EFFECT OF COGNITIVE-BEHAVIORAL GROUP THERAPY ON THE HOPELESS AND LONELINESS AMONG DIVORCED WOMEN

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APA: Copy

KAKHKI, SAMANEH, SHAHOSSEINI, SORAYYA, & ZARGHI, AFSHIN. (2014). DESIGN, SYNTHESIS AND CYTOTOXICITY EVALUATION OF NEW 2-ARYL-5, 6-DIHYDROPYRROLO [2, 1-A]ISOQUINOLINE DERIVATIVES AS TOPOISOMERASE INHIBITORS. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 13(SUPPL), 71-77. SID. https://sid.ir/paper/288411/en

Vancouver: Copy

KAKHKI SAMANEH, SHAHOSSEINI SORAYYA, ZARGHI AFSHIN. DESIGN, SYNTHESIS AND CYTOTOXICITY EVALUATION OF NEW 2-ARYL-5, 6-DIHYDROPYRROLO [2, 1-A]ISOQUINOLINE DERIVATIVES AS TOPOISOMERASE INHIBITORS. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2014;13(SUPPL):71-77. Available from: https://sid.ir/paper/288411/en

IEEE: Copy

SAMANEH KAKHKI, SORAYYA SHAHOSSEINI, and AFSHIN ZARGHI, “DESIGN, SYNTHESIS AND CYTOTOXICITY EVALUATION OF NEW 2-ARYL-5, 6-DIHYDROPYRROLO [2, 1-A]ISOQUINOLINE DERIVATIVES AS TOPOISOMERASE INHIBITORS,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 13, no. SUPPL, pp. 71–77, 2014, [Online]. Available: https://sid.ir/paper/288411/en

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