title: Synthesis and evaluation of 3-amino/guanidine substituted phenyl oxazoles as a novel class of LSD1 inhibitors with anti-proliferative properties.
abstract: A series of functionalized phenyl oxazole derivatives was designed, synthesized and screened in vitro for their activities against LSD1 and for effects on viability of cervical and breast cancer cells, and in vivo for effects using zebrafish embryos. These compounds are likely to act via multiple epigenetic mechanisms specific to cancer cells including LSD1 inhibition.
authors.affiliation: Institut für Organische Chemie, Universität Regensburg, Universitäts str. 31, 93053 Regensburg, Germany.
authors.forename: Balakrishna
authors.initials: B
authors.lastname: Dulla
authors.forename: Krishna Tulasi
authors.initials: KT
authors.lastname: Kirla
authors.forename: Vandana
authors.initials: V
authors.lastname: Rathore
authors.forename: Girdhar Singh
authors.initials: GS
authors.lastname: Deora
authors.forename: Sridhar
authors.initials: S
authors.lastname: Kavela
authors.forename: Subbareddy
authors.initials: S
authors.lastname: Maddika
authors.forename: Kiranam
authors.initials: K
authors.lastname: Chatti
authors.forename: Oliver
authors.initials: O
authors.lastname: Reiser
authors.forename: Javed
authors.initials: J
authors.lastname: Iqbal
authors.forename: Manojit
authors.initials: M
authors.lastname: Pal
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D019791:Guanidine / Q000737:chemistry*; D056466:Histone Demethylases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D056004:Molecular Dynamics Simulation; D015394:Molecular Structure; D010080:Oxazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D015027:Zebrafish
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D010080:Oxazoles; D056466:Histone Demethylases; C495195:KDM1A protein, human; D019791:Guanidine