2. Academic Validation
  3. Structural requirement(s) of N-phenylthioureas and benzaldehyde thiosemicarbazones as inhibitors of melanogenesis in melanoma B 16 cells

Structural requirement(s) of N-phenylthioureas and benzaldehyde thiosemicarbazones as inhibitors of melanogenesis in melanoma B 16 cells

  • Bioorg Med Chem Lett. 2010 May 1;20(9):2991-3. doi: 10.1016/j.bmcl.2010.02.067.
P Thanigaimalai 1,  Tuan Anh Le Hoang,  Ki-Cheul Lee,  Seong-Cheol Bang,  Vinay K Sharma,  Cheong-Yong Yun,  Eunmiri Roh,  Bang-Yeon Hwang,  Youngsoo Kim,  Sang-Hun Jung
Affiliations

Affiliation

  • 1 College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, South Korea.
PMID: 20359890 DOI: 10.1016/j.bmcl.2010.02.067
Abstract

In order to define the structural requirements of phenylthiourea (PTU), a series of thiourea and thiosemicarbazone analogs were prepared and evaluated as inhibitors of melanogenesis in melanoma B16 cells. The most potent analog was 2-(4-tert-butylbenzylidene)hydrazinecarbothioamide (1u) with an IC(50) value of 2.7 microM in inhibition of melanogenesis. The structure for potent inhibitory activity of these derivatives are required with the direct connection of pi-planar structure to thiourea without steric hinderance in PTU derivatives and the hydrophobic substituent at para position in case of semicarbazones.

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