title: Rational design, synthesis and anti-proliferative evaluation of novel benzosuberone tethered with hydrazide-hydrazones.
abstract: Two different series of novel analogues of benzosuberones (5a-m and 9a-w) tethered with hydrazone-hydrazides (functional group alterations: Head group to Tail group and vice versa) have been synthesized by the reaction of appropriate aldehydes with substituted hydrazides in excellent yields (87-94%) and their structures were confirmed by (1)H NMR, (13)C NMR, ESI-MS and HRMS. The newly synthesized compounds were evaluated for anti-proliferative activity against different human cancer cell lines (HeLa, MDA MB 231, MIAPACA and IMR32). Among the synthesized compounds, six compounds 5 a, 5 b, 5 d, 5 e, 5 f and 9 v exhibited potent anti-proliferative activity with GI50 values less than 0.01 μM against MIAPACA, MDA-MB-231 and IMR32 human cancer cell lines.
authors.affiliation: Organic Chemistry Division II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
authors.forename: Bandi
authors.initials: B
authors.lastname: Yadagiri
authors.affiliation: Organic Chemistry Division II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
authors.forename: Uma Devi
authors.initials: UD
authors.lastname: Holagunda
authors.affiliation: Organic Chemistry Division II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
authors.forename: Rajashaker
authors.initials: R
authors.lastname: Bantu
authors.affiliation: Organic Chemistry Division II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India. Electronic address: lnagarapuiict@yahoo.com.
authors.forename: Lingaiah
authors.initials: L
authors.lastname: Nagarapu
authors.affiliation: Organic Chemistry Division II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
authors.forename: Vijayacharan
authors.initials: V
authors.lastname: Guguloth
authors.affiliation: Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
authors.forename: Sowjanya
authors.initials: S
authors.lastname: Polepally
authors.affiliation: Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
authors.forename: Nishanth
authors.initials: N
authors.lastname: Jain
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D006367:HeLa Cells; D006801:Humans; D006834:Hydrazines / Q000737:chemistry*; D006835:Hydrazones / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D003374:Coumarins; D006834:Hydrazines; D006835:Hydrazones; C000594239:benzosuberone; C029424:hydrazine
keywords: Anti-proliferative; Benzosuberone; Cell lines; Hydrazide–hydrazones