Corina Cheptea1, Valeriu Sunel2, Ana Cezarina Morosanu3, Dan Gheorghe Dimitriu3, Mihaela Maria Dulcescu-Oprea4, Mihai-Daniel Angheluta5, Mihaela Miron6, Cristina Delia Nechifor7, Dana Ortansa Dorohoi3, Razvan Nicolae Malancus8. 1. Department of Biomedical Sciences, Faculty of Biomedical Engineering, "Grigore T. Popa" University of Medicine and Pharmacy, 700115 Iasi, Romania. 2. Faculty of Chemistry, Alexandru Ioan Cuza University, 700506 Iasi, Romania. 3. Faculty of Physics, Alexandru Ioan Cuza University, 700506 Iasi, Romania. 4. Regional Institute of Oncology, 700483 Iasi, Romania. 5. Faculty of Medicine, "Iuliu Hateganu" University of Medicine and Pharmacy, 400012 Cluj-Napoca, Romania. 6. Faculty of Medicine, "Grigore T. Popa" University of Medicine and Pharmacy, 700115 Iasi, Romania. 7. Department of Physics, Faculty of Machine Manufacturing and Industrial Management, 700050 Iasi, Romania. 8. Department of Physiology and Pathophysiology, Faculty of Veterinary Medicine, "Ion Ionescu de la Brad" University of Agricultural Sciences and Veterinary Medicine, 700490 Iasi, Romania.
Abstract
New di-(β-chloroethyl)-amides of some acids derived from 2-mercaptobenzoxazole were prepared by reaction of the corresponding pivalic mixed anhydrides with di-(β-chloroethyl)-amine. A study regarding the optimization of the chemical reactions was made for the case of di-(β-chloroethyl)-amines. The quantum chemical analysis by Spartan'14 was made in order to establish the most stable configuration of the ground electronic states for the obtained chemical structures and some physico-chemical parameters of N-mustards reported in this paper. Mercaptobenzoxazoles substituted in the side chain with the cytotoxic group show antitumor activity and they inhibit Ehrlich Ascites in an appreciable proportion compared to the drug I.O.B.-82, as our studies evidenced.
New di-(β-chloroethyl)-n class="Chemical">amides of some acids derived from 2-mercaptobenzoxazole were prepared by reaction of the corresponding pivalic mixed anhydrides with di-(β-chloroethyl)-amine. A study regarding the optimization of the chemical reactions was made for the case of di-(β-chloroethyl)-amines. The quantum chemical analysis by Spartan'14 was made in order to establish the most stable configuration of the ground electronic states for the obtained chemical structures and some physico-chemical parameters of N-mustards reported in this paper. Mercaptobenzoxazoles substituted in the side chain with the cytotoxic group show antitumor activity and they inhibit Ehrlich Ascites in an appreciable proportion compared to the drug I.O.B.-82, as our studies evidenced.
Authors: M C Viaud; P Jamoneau; C Flouzat; J G Bizot-Espiard; B Pfeiffer; P Renard; D H Caignard; G Adam; G Guillaumet Journal: J Med Chem Date: 1995-04-14 Impact factor: 7.446
Authors: T Yakaiah; B P V Lingaiah; B Narsaiah; B Shireesha; B Ashok Kumar; S Gururaj; T Parthasarathy; B Sridhar Journal: Bioorg Med Chem Lett Date: 2007-03-30 Impact factor: 2.823