Design, synthesis, and anticancer evaluation of some novel thiourea, carbamimidothioic acid, oxazole, oxazolidine, and 2-amino-1-phenylpropyl-2-chloroacetate derived from L-norephedrine

作者：Abdel Kader Maged S; Ghorab Mostafa M^*; Alsaid Mansour S; Alqasoumi Saleh I

来源：Russian Journal of Bioorganic Chemistry, 2016, 42(4): 434-440.

DOI：10.1134/S1068162016040026

• thiourea carbamimidothioic acid
• oxazole
• oxazolidine
• 2-amino-1-phenylpropyl-2-chloroacetate
• anticancer activity

A novel series of thiourea, carbamimidothioic acid, 4, 5-dihydrooxazole-2-thiol, oxazolidine-2thine, and 2-amino-1-phenylpropyl-2-chloroacetate derivatives was designed and synthesized using 2-amino-1-phenylpropan-1-ol (L-norephedrine) as a strategic starting material. The structures of the newly synthesized compounds were established by elemental analyses, IR, and H-1 NMR and C-13 NMR spectral data. The compounds were evaluated for their in vitro anticancer activity against various cancer cell lines. The corresponding acetamide, carbamimidothioic acid, and 2-2-amino-1-phenylpropyl-2-chloroacetate derivatives showed almost the same activity as the standard drug doxorubicin against human breast cancer cell line (MCF-7). Also, the acetamide and 2-thioxoimidazolidin-4-one derivatives exhibited higher activity than the reference drug doxorubicin against human colon cancer cell line (HCT 116).

• 出版日期2016-7