Dergiler / Organic Communications / 2022 / Cilt: 15 - Sayı: 2

Design, synthesis, in silico and biological evaluation of biotinpyrazole derivatives as cytotoxic agent Rahul

Sayfa
117–128
DOI
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⚡ TL;DR(1 Cümlede Hızlı Çıkarım)

Among target agents, 3a had a considerable activity against human brain cancer cell line U251 (IC50 3.5 μM). 3a could be a promising candidate for the development of new drugs to treat tumours, particularly for brain cancer.

📌 3 Maddede Bu Makale

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Amaç & Hipotez:Modified biotin derivatives are effective in killing cancer.
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Temel Bulgular & Veri:Herein we describe the design and synthesis of conjugated biotin-pyrazole derivatives 3a-3h to evaluate as potential anticancer agents.
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Sonuç & Katkı:Among target agents, 3a had a considerable activity against human brain cancer cell line U251 (IC50 3.5 μM). 3a could be a promising candidate for the development of new drugs to treat tumours, particularly for brain cancer.
🔬Tür:Araştırma Makalesi
📍Kapsam:Genişletilmiş Akademik Örneklem
⚙️Değişkenler:Alan Parametreleri

Özet

Modified biotin derivatives are effective in killing cancer. Herein we describe the design and synthesis of conjugated biotin-pyrazole derivatives 3a-3h to evaluate as potential anticancer agents. A set of compounds has been prepared by palladium catalysed aminocarbonylation using carbon monoxide in an autoclave. They were well characterized by various spectroscopic techniques and screened for anticancer activity. A cell viability assay (MTT assay) was performed on U251, A549, and HepG2 cell lines and determined their IC50 value. Among target agents, 3a had a considerable activity against human brain cancer cell line U251 (IC50 3.5 μM). 3a could be a promising candidate for the development of new drugs to treat tumours, particularly for brain cancer.

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Bu Makaleye Atıf Yap

RAYANİ, R., SONİ, J. Y., PARMAR, D. R., KUSURKAR, R. V., VALA, A., ZUNJAR, V., BATTULA, S. (2022). Design, synthesis, in silico and biological evaluation of biotinpyrazole derivatives as cytotoxic agent Rahul. Organic Communications, Cilt: 15 - Sayı: 2, 117–128. https://ajindex.com/articles/417557

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Kaynakça (13)

  1. Parmar, D. R.; Soni, J. Y.; Guduru, R.; Rayani, R. H.; Kusurkar, R.V.; Vala, Talukdar, S.N.; Eissa, İ.H.; Metwal, A.M.; Khalil, A.; Zunjar, V.; Battula, S. Discovery of new anticancer thiourea-azetidine hybrids: design, synthesis, in vitro antiproliferative, SAR, in silico molecular docking against VEGFR-2, ADMET, toxicity, and DFT studies. Bioorg. Chem. 2021, 115, 105206
  2. Cancer Facts & Figures (2013). http://www.cancer.org/research/cancerfactsstatistics-/cancerf actsfigures2013/ [3] Bolden, E.; Peart, J.; Johnstone, W. Anticancer activities of histone deacetylase inhibitors. Nat. Rev. Drug Discov. 2006, 5, 769-784
  3. Dumontet, C.; Jordan, A.; Microtubule-binding agents: a dynamic field of cancer therapeutics. Nat. Rev. Drug Discov. 2010, 9, 790-803
  4. Gibiansky, L.; Gibiansky, E.; Target-mediated drug disposition model and its approximations for antibody-drug conjugates. J. Pharmacokinet. Pharmacodyn. 2014, 41, 35-47
  5. Bareford,M.; Avaritt. R.; Ghandehari, H.; Nan, A.; Swaan. W.; Riboflavintargeted polymer conjugatesfor breast tumor delivery. Pharm. Res. 2013, 30, 1799-1812
  6. Altaner, C.; Altanerova, V.; Cihova, M.; Ondicova, K.; Rychly, B. Complete regression of glioblastoma by mesenchymal stem cells mediated prodrug gene therapy simulating clinical therapeutic scenario. Int. J. Cancer 2014, 134, 1458-1465
  7. Elsadek, B.; Graeser, R.; Esser, N.; Schäfer-Obodozie, C.; Abu Ajaj, K. Development of a novel prodrug of paclitaxel that is cleaved by prostate-specific antigen: An in vitro and in vivo evaluation study. Eur. J. Cancer 2010, 46, 3434-3444
  8. Said, M. Biotin: The forgotten vitamin, Am. J. Clin. Nutr. 2002,75, 179–80
  9. Bildstein, L.; Dubernet,C.; Couvreur, P. Adv. Drug Delivery Rev. 2011, 63, 3-23
  10. Maiti, S.; Paira, P. Biotin conjugated organic molecules and proteins for cancer therapy: A review. Eur J. Med. Chem. 2018, 145, 206-223
  11. Russell-Jones, G.; McTavish,K.; McEwan, J.; Rice J.; Nowotnik, D. Vitamin-mediated targeting as a potential mechanism to increase drug uptake by tumours. J. Inorg. Biochem. 2004, 98, 1625 - 1633
  12. Tripodo, G.; Mandracchia,D.; Collina,S.; Rui, M.; Rossi, D. New perspectives in cancer therapy: the biotin-antitumor molecule conjugates, Med. Chem. 2014, S1: 004. (8 pages).doi:10.4172/2161-0444
  13. Fatima, A.; Mohemmed, FK.; Wasim, A.; Mohammad, MA.; Lalit. M,; Sumit, K.; Mymoona, A.; Suhel, P.;Syed, MH.; Mohammad S.; Revealing quinquennial anticancer journey of morpholine: A SAR bas