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Synthesis of New Heterocyclic Amino Derivatives of Alantolactone and Their Cytotoxic Activity
Author(s) -
Kumar Ashish,
Kumar Dharmesh,
Maurya Antim K.,
Padwad Yogendra S.,
Agnihotri Vijai K.
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.3328
Subject(s) - chemistry , cytotoxicity , epidermoid carcinoma , adduct , stereochemistry , in vitro , cytotoxic t cell , in vivo , cell culture , amino acid , cancer cell , cancer , biochemistry , organic chemistry , genetics , biology
In this study, a series of new alantolactone ( AL ) amino scaffolds ( AL1 – AL13 ) had been synthesized and evaluated for in vitro cytotoxicity against three human cancer cell lines: human cervical cancer (SiHa), human epidermoid carcinoma (KB), and human lung cancer (A549). The compounds AL 2 , 4 , 5 , 7 , and 13 were found to be nearly as equally active as AL against three tested cell lines, whereas AL 1 and 12 against SiHa cells. This study also provides a correlation on the structure activity relationship of AL and derivatized analogues against tested cells. The retention of cytotoxicity with enhanced water solubility in derivatized amino adducts including AL 1 , 2 , 4 , 5 , 7 , 12 , and 13 indicates that these adducts can further be tested for the detailed in vivo safety and anticancer studies.