Synthesis and Cytotoxicity Evaluation of Novel Andrographolide‐1,2,3‐Triazole Derivatives |
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| Authors: | Yakaiah Chinthala Manjulatha K Pooja Sharma Satya Srinivas Kvn Kotesh Jonnala Niranjana Kumar Arigari Feroz Khan Setty Oh |
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| Institution: | 1. Natural Product Chemistry, CSIR‐Central Institute of Medicinal and Aromatic Plants‐Research Centre, Hyderabad, Telangana, India;2. Department of Biochemistry, School of Life Sciences, University of Hyderabad, India;3. Metabolic and Structural Biology Department, CSIR‐Central Institute of Medicinal and Aromatic Plants, Lucknow, Uttar Pradesh, India |
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| Abstract: | 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. |
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