SYNTHESIS, SPECTRAL CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF NOVEL THIAZOLE-OXOINDOLE HYBRID COMPOUNDS AS POTENTIAL ANTICANCER AGENTS
El-Sharief, A., Ammar, Y., El-Sharief, A., Mohamed, Y., Mehany, A., Ragab, A. (2018). SYNTHESIS, SPECTRAL CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF NOVEL THIAZOLE-OXOINDOLE HYBRID COMPOUNDS AS POTENTIAL ANTICANCER AGENTS. EKB Journal Management System, 2018(12), 25-37. doi: 10.21608/absb.2018.33767
A. El-Sharief; Yousry A. Ammar; A. M. El-Sharief; Yehia A. Mohamed; Ahmed B. Mehany; Ahmed Ragab. "SYNTHESIS, SPECTRAL CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF NOVEL THIAZOLE-OXOINDOLE HYBRID COMPOUNDS AS POTENTIAL ANTICANCER AGENTS". EKB Journal Management System, 2018, 12, 2018, 25-37. doi: 10.21608/absb.2018.33767
El-Sharief, A., Ammar, Y., El-Sharief, A., Mohamed, Y., Mehany, A., Ragab, A. (2018). 'SYNTHESIS, SPECTRAL CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF NOVEL THIAZOLE-OXOINDOLE HYBRID COMPOUNDS AS POTENTIAL ANTICANCER AGENTS', EKB Journal Management System, 2018(12), pp. 25-37. doi: 10.21608/absb.2018.33767
El-Sharief, A., Ammar, Y., El-Sharief, A., Mohamed, Y., Mehany, A., Ragab, A. SYNTHESIS, SPECTRAL CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF NOVEL THIAZOLE-OXOINDOLE HYBRID COMPOUNDS AS POTENTIAL ANTICANCER AGENTS. EKB Journal Management System, 2018; 2018(12): 25-37. doi: 10.21608/absb.2018.33767

SYNTHESIS, SPECTRAL CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF NOVEL THIAZOLE-OXOINDOLE HYBRID COMPOUNDS AS POTENTIAL ANTICANCER AGENTS

Al-Azhar Bulletin of Science
Article 3, Volume 2018, Issue 12, December 2018, Pages 25-37    PDF (753.79 K)
Document Type: Original Article
DOI: 10.21608/absb.2018.33767
Authors
A. El-Sharief1; Yousry A. Ammar* 2; A. M. El-Sharief1; Yehia A. Mohamed3; Ahmed B. Mehany4; Ahmed Ragab1
1Chemistry Department, Faculty of Science, Al-Azhar University, Nasr City, Cairo, 11284, Egypt
2Chemistry Department, Faculty of Science, Al-Azhar University, Nasr City, Cairo, 11284, Egypt.
31Chemistry Department, Faculty of Science, Al-Azhar University, Nasr City, Cairo, 11284, Egypt
4Zoology Department, Faculty of Science, Al-Azhar University, Nasr City, Cairo, 11284, Egypt
Abstract
In the present study, a series of thiazole derivatives bearing 5-morpholinosulfonylindole were designed and synthesized through condensation of 5-(morpholinosulfonyl)isatin (1) with some thiazolidinone derivatives as carbon nucleophiles to afford the corresponding arylidene derivatives (2-5, 7, 8). Furthermore, many thiazole derivatives (11-15) were obtained through the reaction of thiosemicarbazone derivative (10) with many reagents such as dimethyl acetelenedicarboxylate, phencylbromide derivatives, chloroacetonitrile, chloroacetylchloride as well as chloroacetanilide. The newly synthesized compounds were characterized based on spectral (FT-IR,1H NMR, 13C NMR, MS) analysis. Cytotoxicity effects of all synthesized products were tested against three cancer cell lines, MCF-7, HepG-2, HCT-116 and they showed moderate to good cytotoxic activity against the three tested cell lines. The study showed that compounds (2a, 12b and 12c) were less or almost equipotent as doxorubicin against the three cell lines HepG-2, HCT-116.
Keywords
Isatin; thiazol-4(5H)-one; 4-thiazolidinone; thiosemicarbazone derivatives
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