title: Synthesis and Selective Cytotoxic Activities on Rhabdomyosarcoma and Noncancerous Cells of Some Heterocyclic Chalcones.
abstract: Chemically diverse heterocyclic chalcones were prepared and evaluated for cytotoxicity, aiming to push forward potency and selectivity. They were tested against rhabdomyosarcoma (RMS) and noncancerous cell line (LLC-PK1). The influence of heteroaryl patterns on rings A and B was studied. Heterocycle functionalities on both rings, such as phenothiazine, thiophene, furan and pyridine were evaluated. Notably, the introduction of three methoxy groups at positions 3, 4, 5 on ring B appears to be critical for cytotoxicity. The best compound, with potent and selective cytotoxicity (IC50 = 12.51 μM in comparison with the value 10.84 μM of paclitaxel), contains a phenothiazine moiety on ring A and a thiophene heterocycle on ring B. Most of the potential compounds only show weak cytoxicity on the noncancerous cell line LLC-PK1.
authors.affiliation: Faculty of Applied Sciences, Ton Duc Thang University, 19 Nguyen Huu Tho St., Tan Phong Ward, Dist. 7, Ho Chi Minh City 700000, Vietnam. dotuongha@tdt.edu.vn.
authors.forename: Tuong-Ha
authors.initials: TH
authors.lastname: Do
authors.affiliation: Faculty of Pharmacy, University of Medicine and Pharmacy, Ho Chi Minh City, 41 Dinh Tien Hoang St., Dist. 1, Ho Chi Minh City 700000, Vietnam. nguyendaiminh.medchem@gmail.com.
authors.forename: Dai-Minh
authors.initials: DM
authors.lastname: Nguyen
authors.affiliation: Faculty of Pharmacy, University of Medicine and Pharmacy, Ho Chi Minh City, 41 Dinh Tien Hoang St., Dist. 1, Ho Chi Minh City 700000, Vietnam. dattv.vn@gmail.com.
authors.forename: Van-Dat
authors.initials: VD
authors.lastname: Truong
authors.affiliation: Faculty of Pharmacy, University of Medicine and Pharmacy, Ho Chi Minh City, 41 Dinh Tien Hoang St., Dist. 1, Ho Chi Minh City 700000, Vietnam. hongtuoid99@gmail.com.
authors.forename: Thi-Hong-Tuoi
authors.initials: TH
authors.lastname: Do
authors.affiliation: Faculty of Pharmacy, University of Medicine and Pharmacy, Ho Chi Minh City, 41 Dinh Tien Hoang St., Dist. 1, Ho Chi Minh City 700000, Vietnam. leminhtri1099@gmail.com.
authors.forename: Minh-Tri
authors.initials: MT
authors.lastname: Le
authors.affiliation: Faculty of Chemical Engineering, Ho Chi Minh City University of Technology, Vietnam National University, Ho Chi Minh City, 268 Ly Thuong Kiet St, Dist. 10, Ho Chi Minh City 700000, Vietnam. ptquan@hcmut.edu.vn.
authors.forename: Thanh-Quan
authors.initials: TQ
authors.lastname: Pham
authors.affiliation: Faculty of Pharmacy, University of Medicine and Pharmacy, Ho Chi Minh City, 41 Dinh Tien Hoang St., Dist. 1, Ho Chi Minh City 700000, Vietnam. thaikhacminh@uphcm.edu.vn.
authors.forename: Khac-Minh
authors.initials: KM
authors.lastname: Thai
authors.affiliation: Faculty of Pharmacy, University of Medicine and Pharmacy, Ho Chi Minh City, 41 Dinh Tien Hoang St., Dist. 1, Ho Chi Minh City 700000, Vietnam. thaikhacminh@gmail.com.
authors.forename: Thanh-Dao
authors.initials: TD
authors.lastname: Tran
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D012208:Rhabdomyosarcoma / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D013552:Swine
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones; D006571:Heterocyclic Compounds
keywords: LLC-PK1 cell; MTT; cytotoxicity; heterocyclic chalcones; rhabdomyosarcoma