title: Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents.
abstract: A new series of 1,3-biarylsulfanyl derivatives (homodibenzyl core motif) have been designed and synthesized as new estrogen receptor ligands by chopping benzothiophene core of raloxifene to engender seco-raloxifene scaffold. All the synthesized compounds were screened for anti-proliferative, anti-osteoporotic, and anti-implantation activity. Compounds (35, 36) having basic amino anti-estrogenic side chain were exhibiting potential anti-proliferative activity in MCF-7, MDA-MB-231 and ishikawa cell lines. Some of the synthesized compounds having homodibenzyl motif (5, 8, 10) have shown moderate anti-osteoporotic activity.
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226 001, India. dratulsax@gmail.com
authors.forename: Atul
authors.initials: A
authors.lastname: Kumar
authors.forename: Vishwa Deepak
authors.initials: VD
authors.lastname: Tripathi
authors.forename: Promod
authors.initials: P
authors.lastname: Kumar
authors.forename: Lalit Prakash
authors.initials: LP
authors.lastname: Gupta
authors.lastname: Akanksha
authors.forename: Ritu
authors.initials: R
authors.lastname: Trivedi
authors.forename: Hemant
authors.initials: H
authors.lastname: Bid
authors.forename: V L
authors.initials: VL
authors.lastname: Nayak
authors.forename: Jawed A
authors.initials: JA
authors.lastname: Siddiqui
authors.forename: Bandana
authors.initials: B
authors.lastname: Chakravarti
authors.forename: Ruchi
authors.initials: R
authors.lastname: Saxena
authors.forename: Anila
authors.initials: A
authors.lastname: Dwivedi
authors.forename: M I
authors.initials: MI
authors.lastname: Siddiquee
authors.forename: U
authors.initials: U
authors.lastname: Siddiqui
authors.forename: Rituraj
authors.initials: R
authors.lastname: Konwar
authors.forename: Naibedya
authors.initials: N
authors.lastname: Chattopadhyay
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005260:Female; D057809:HEK293 Cells; D006801:Humans; D008958:Models, Molecular; D008968:Molecular Conformation; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D013438:Sulfhydryl Compounds