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Design and Synthesis of New Etodolac‐Pyridazinones as Potent Anticancer Agents Using Pb(OAc) 4 to Assist N‐N Bond Formation
Author(s) -
Kummari Bhaskar,
Ramesh Perla,
Parsharamulu Rayam,
Allaka Tejeswara Rao,
Anantaraju Hasithashilpa,
Yogeeswari Perumal,
Balasubramanian Sridhar,
Guggilapu Sravanthi Devi,
Babu Bathini Nagendra,
Anireddy Jaya Shree
Publication year - 2018
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201800459
Subject(s) - chemistry , hydrazide , stereochemistry , in vitro , potency , molecule , cytotoxic t cell , combinatorial chemistry , biochemistry , organic chemistry
Pb(OAc) 4 to assist N−N bond formation via dehydrogenative cyclization of hydrazide‐hydrazones to generate the pyridazinones as bioactive molecules have been described. All the products were well characterized by various spectroscopic analyses. Furthermore, the structure of ( E )‐3a,7‐diethyl‐6‐((thiophen‐2‐ylmethylene)amino)‐1,2,3a,4‐tetrahydro‐3‐oxa‐6,6a‐diazafluoranthen‐5(6H)‐one was unambiguously conformed by single crystal X‐ray analysis. The in vitro biological evaluation revealed that several of these compounds exhibited greater cytotoxic potency than that of doxorubicin drug. ( E )‐N′‐(4‐chlorobenzylidene)‐2‐(1,8‐diethyl‐1,3,4,9‐tetrahydropyrano[3,4‐b]indol‐1‐yl)acetohydrazide exhibited most cytotoxic activity against both A549 and PC3 cancer cell lines with IC 50 values of 1.77±0.08 and 1.88±0.33 μM, respectively.