Design, synthesis and biological evaluation of oxime lacking Psammaplin inspired chemical libraries as anti-cancer agents

被引:4
作者
Kumar, Srinivas Lavanya M. [1 ]
Ali, Kasim [1 ]
Chaturvedi, Priyank [2 ]
Meena, Sanjeev [2 ]
Datta, Dipak [2 ]
Panda, Gautam [1 ]
机构
[1] Cent Drug Res Inst, CSIR, Med & Proc Chem Div, Sitapur Rd, Lucknow 226031, UP, India
[2] Cent Drug Res Inst, CSIR, Canc Biol Div, Sitapur Rd, Lucknow 226031, UP, India
关键词
Psammaplin; Colon cancer; Structure-activity relationship (SAR) study; Ideal reaction condition; Cytotoxic; MARINE NATURAL-PRODUCT; HISTONE DEACETYLASE; ANALOGS; METABOLITES; INHIBITION; DISCOVERY;
D O I
10.1016/j.molstruc.2020.129173
中图分类号
O64 [物理化学(理论化学)、化学物理学];
学科分类号
070304 ; 081704 ;
摘要
In this study, we attempted the chemical simplification of Psammaplin (PsA), while retaining its activity in vitro . Inspired by the previous Structure Activity Relationship (SAR) studies on various PsA analogues and relying on the fact that oxime is metabolically unstable, we initially designed and synthesized a diverse library of PsA analogues and evaluated for cytotoxic activity. Among 32 compounds of Psammaplin analogues synthesized, the compound 10b was almost equally active as parent Psammaplin in vitro. (C) 2020 Elsevier B.V. All rights reserved.
引用
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页数:14
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