Synthesis of functionalized amino acid derivatives as new pharmacophores for designing anticancer agents.
A new series of functionalized amino acid derivatives N-substituted 1-N-(tert-butoxycarbonyl)-2,2-dimethyl-4-phenyl-5-oxazolidine carboxamide (1-17) and 1-N-substituted-3-amino-2-hydroxy-3-phenylpropane-1-carboxamide (18-34) were synthesized and evaluated for their in vitro cytotoxicity against human cancer cell lines. Compound 6 has shown interesting cytotoxicity (IC(50) = 5.67 microm) in ovarian cancer, while compound 10 exhibited promising cytotoxicity in ovarian (IC(50) = 6.1 microm) and oral (IC(50) = 4.17 microm) cancers. These compounds could be of use in designing new anti-cancer agents.
Kumar
Vivek
V
Chemical Research, Dabur Research Foundation, 22, Site IV, SahibabadGhaziabad, 201 010, UP, India. kumarv@dabur.com
Mudgal
Mukesh M
MM
Rani
Nidhi
N
Jha
Amrita
A
Jaggi
Manu
M
Singh
Anu T
AT
Sanna
Vinod K
VK
Singh
Pratibha
P
Sharma
Pramod K
PK
Irchhaiya
Raghuveer
R
Burman
Anand C
AC
D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000596:Amino Acids / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D045744:Cell Line, Tumor; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005260:Female; D005347:Fibroblasts / Q000166:cytology / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D009062:Mouth Neoplasms / Q000473:pathology; D010051:Ovarian Neoplasms / Q000473:pathology
D000577:Amides; D000596:Amino Acids; D000970:Antineoplastic Agents