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Design, Synthesis and SAR Study of Novel Spiro [Pyrimido[5,4‐b]Quinoline‐10,5′‐Pyrrolo[2,3‐d]Pyrimidine] Derivatives as Promising Anticancer Agents
Author(s) -
Chate Asha V.,
Kamdi Sagar P.,
Bhagat Amruta N.,
Jadhav Chetan K.,
Nipte Amol,
Sarkate Aniket P.,
Tiwari Shailee V.,
Gill Charansingh H.
Publication year - 2018
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3286
Subject(s) - chemistry , quinoline , pyrimidine , stereochemistry , mtt assay , in vitro , hela , combinatorial chemistry , mcf 7 , cancer cell , cancer , human breast , biochemistry , organic chemistry , medicine
Novel spiro [pyrimido[5,4‐b]quinoline‐10,5′‐pyrrolo[2,3‐d]pyrimidine] derivatives were designed and synthesized, and their chemical structures were confirmed by IR, NMR, elemental analysis, and mass spectral analysis. The anticancer activities of the newly synthesized compounds were evaluated in vitro against four human cancer cell lines including A431, PC‐3, MCF‐7, and MCF‐10A by MTT assay. The screening results showed that three compounds ( 4m , 4q , and 4s ) exhibited potent cytotoxic activities with IC 50 values between 7.82 and 9.88 μM against human breast cancer cell line (MCF‐7). Further in vitro studies revealed that inhibition of Sunitinib could be the possible mechanism of action of these molecules.