Synthesis and anticancer activities of novel (tetrahydrobenzo [4,5] thieno [2,3-d] pyrimidine-4-yl)-pyrolidine-2-carboxylic acid derivatives

被引:14
|
作者
Pavase, Laxmikant S. [1 ]
Mane, Dhananjay V. [1 ]
机构
[1] Dr Babasaheb Ambedkar Marathwada Univ, Dept Chem, Aurangabad 431004, Maharashtra, India
关键词
Thieno pyrimidine; Proline; Gewald reaction; MCF-7; HCT-15; Antitumor activities; LUNG-CANCER; AGENTS;
D O I
10.1007/s00044-016-1692-x
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Cancer chemotherapy has been one of the major medical advances in the last few decades. The medications involved in treatment have a narrow therapeutic index, and often the responses produced are only just palliative as well as unpredictable. In contrast, targeted therapy such as Tyrosine kinases inhibitors, that has been introduced in recent years is directed against cancer-specific molecules and signaling pathways with some side effects Therefore, we studied these class of molecules to obtain new candidates of remarkable activities and minimal side effects. We herein reported SAR driven synthesis of 16 novel molecules and their anticancer profiles in specifically targeted human Breast cell line MCF-7 and Human Colon Cancer Cell Line HCT-15. Compounds 7e and 8f showed descent antitumor activities when compared to Doxorubicine (GI(50) < 0.1) for human Breast cell line MCF-7. The synthesized analogs were ensured by spectral and elemental analysis.
引用
收藏
页码:2380 / 2391
页数:12
相关论文
共 50 条
  • [31] NEW THIENO COMPOUNDS .14. SYNTHESIS OF 4-AMINO-SUBSTITUTED THIENO[2,3-D]PYRIMIDINE-6-CARBOXYLIC ACID-DERIVATIVES
    BAUMGARTNER, A
    PECH, R
    BOHM, R
    PHARMAZIE, 1993, 48 (03): : 192 - 194
  • [32] Targeted Synthesis and Study of Anti-tyrosinase Activity of 2-Substituted Tetrahydrobenzo[4,5]Thieno[2,3-d]Pyrimidine-4(3H)-One
    Chiriapkin, Alexey
    Kodonidi, Ivan
    Pozdnyakov, Dmitry
    IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH, 2022, 21 (01):
  • [33] A facile synthesis of some thieno/furo-[2,3-d]pyrimidine-2-yl-thioacetic acid derivatives
    Demirayak, S
    Abu Mohsen, U
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 2001, 38 (02) : 507 - 509
  • [34] Synthesis and antiproliferative evaluation of novel tetrahydrobenzo[4′,5′]thieno[3′,2′:5,6]pyrido[4,3-d] pyrimidine derivativest
    Tang, Chu
    Liang, Yongju
    Bai, Shun
    He, Hongwu
    Chen, Yu
    Yang, Guangzhong
    Fu, Liwu
    RSC ADVANCES, 2014, 4 (55) : 29187 - 29192
  • [35] Novel synthesis of thieno[2,3-c]pyridazine and pyrimido[4′,5′:4,5]thieno[2,3-c]pyridazine derivatives
    El-Dean, AMK
    El-Gaby, MSA
    Gaber, AM
    Eyada, HA
    Al-Kamali, ASN
    PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, 2005, 180 (02) : 413 - 424
  • [36] Synthesis of New 5-(1,4-Benzodioxan-2-yl)thieno[2,3-d]pyrimidine Derivatives
    S. O. Vardanyan
    A. A. Aghekyan
    A. S. Avagyan
    A. B. Sargsyan
    H. A. Panosyan
    S. A. Harutyunyan
    H. V. Gasparyan
    Russian Journal of Organic Chemistry, 2022, 58 : 977 - 981
  • [37] Synthesis of New 5-(1,4-Benzodioxan-2-yl)thieno[2,3-d]pyrimidine Derivatives
    Vardanyan, S. O.
    Aghekyan, A. A.
    Avagyan, A. S.
    Sargsyan, A. B.
    Panosyan, H. A.
    Harutyunyan, S. A.
    Gasparyan, H., V
    RUSSIAN JOURNAL OF ORGANIC CHEMISTRY, 2022, 58 (07) : 977 - 981
  • [38] SYNTHESIS OF (2,3-D)-THIENO-PYRIMIDINE AND OF SOME DERIVATIVES
    ROBBA, M
    LECOMTE, JM
    DESEVRIC.MC
    COMPTES RENDUS HEBDOMADAIRES DES SEANCES DE L ACADEMIE DES SCIENCES SERIE C, 1968, 266 (02): : 128 - &
  • [39] SYNTHESIS OF NEW THIENO[2,3-D] PYRIMIDINE-DERIVATIVES
    IBRAHIEM, LI
    TAMMAM, GH
    ABDIN, TMS
    JOURNAL OF THE CHEMICAL SOCIETY OF PAKISTAN, 1989, 11 (03): : 227 - 231
  • [40] Synthesis and Cytotoxicity of Some Thieno[2,3-d]pyrimidine Derivatives
    Saddik, Abdelreheem A.
    El-Dean, Adel M. Kamal
    El-Sokary, Gamal H.
    Hassan, Khairy M.
    Abbady, Mohamed S.
    Ismail, Ismail A.
    Saber, Saber H.
    JOURNAL OF THE CHINESE CHEMICAL SOCIETY, 2017, 64 (01) : 87 - 93