Synthesis and Cytotoxicity Evaluation of Novel Andrographolide-1,2,3-Triazole Derivatives

A series of new andrographolide‐1,2,3‐triazole derivatives, 3a, 3b, 3c, 3d, 3e, 3f, 3g, 3h, 3i, 3j, 3k, were synthesized from a natural bioactive labdane type diterpenoid, andrographolide. All the derivatives were screened against human cancer cell lines MCF7, MDA‐MB‐231, COLO205, HepG2, K562, Hela,...

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Published inJournal of heterocyclic chemistry Vol. 53; no. 6; pp. 1902 - 1910
Main Authors Chinthala, Yakaiah, K, Manjulatha, Sharma, Pooja, Kvn, Satya Srinivas, Jonnala, Kotesh, Arigari, Niranjana Kumar, Khan, Feroz, Oh, Setty
Format Journal Article
LanguageEnglish
Published HOBOKEN Blackwell Publishing Ltd 01.11.2016
Wiley
Wiley Subscription Services, Inc
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
ALPHA
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Summary:A series of new andrographolide‐1,2,3‐triazole derivatives, 3a, 3b, 3c, 3d, 3e, 3f, 3g, 3h, 3i, 3j, 3k, were synthesized from a natural bioactive labdane type diterpenoid, andrographolide. All the derivatives were screened against human cancer cell lines MCF7, MDA‐MB‐231, COLO205, HepG2, K562, Hela, and HEK293 to evaluate their cytotoxic activity. All the compounds showed anticancer activity selectively against K562 cell line, with IC50 values ranging from 8.00 to 17.11 µM, and are inactive against the rest of the cell lines. Compounds 3c and 3d showed significant cytotoxicity among the synthesized derivatives. The in silico docking studies revealed compounds 3b and 3d with high binding affinity against the cancer target, transient receptor potential vanilloid 1.
Bibliography:Supporting info item
ArticleID:JHET2505
istex:4218AA6172A9873CE0F51A296CBA7F59DE2B7EBB
ark:/67375/WNG-5SPB51FR-4
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.2505