135733-30-1Relevant articles and documents
Design, synthesis and biological study of hybrid drug candidates of nitric oxide releasing cucurbitacin-inspired estrone analogs for treatment of hepatocellular carcinoma
Abou-Salim, Mahrous A.,Shaaban, Mohamed A.,Abd El Hameid, Mohammed K.,Elshaier, Yaseen A.M.M.,Halaweish, Fathi
, p. 515 - 533 (2019)
Development of hybrid drug candidates is well known strategy for designing antitumor agents. Herein, a novel class of nitric oxide donating cucurbitacin inspired estrone analogs (NO-CIEAs) were designed and synthesized as multitarget agents. Synthesized analogs were initially evaluated for their anti-hepatocellular carcinoma activities. Among the tested analogs, NO-CIEAs 17 and 20a exhibited more potent activity against HepG2 cells (IC50 = 4.69 and 12.5 μM, respectively) than the reference drug Erlotinib (IC50 = 25 μM). Interestingly, NO-CIEA 17 exerted also a high potent activity against Erlotinib-resistant HepG2 cell line (HepG2-R) (IC50 = 8.21 μM) giving insight about its importance in drug resistance therapy. Intracellular measurements of NO revealed that NO-CIEAs 17 and 20a showed a significant increase in NO production in tumor cells after 1 h of incubation comparable to the reference prodrug JS-K. Flow cytometric analysis showed that both NO-CIEAs 17 and 20a mainly arrested the HepG2 cells in the G0/G1 phase. Also, In-Cell Based ELISA screening showed that NO-CIEA 17 resulted in a potential inhibitory activity towards the EGFR and MAPK (25% and 29% inhibition compared to untreated control cells, respectively). This data suggests the binding ability of NO-CIEA 17 to the EGFR and ERK to be well correlated along with the docking and cellular studies. Also, treatment of HepG2-R cells with NO-CIEA 17 showed a potential reduction of MRP2 expression in a dose dependent manner providing a significant impact on the chemotherapeutic resistance. Overall, the current study provides a potential new approach for the discovery of a novel antitumor agent against HCC.
A surprising new route to 4-nitro-3-phenylisoxazole
Hopf, Henning,Mourad, Aboul-Fetouh E.,Jones, Peter G.
, (2010)
A one-pot synthesis of 4-nitro-3-phenylisoxazole has been carried out by treatment of cinnamyl alcohol dissolved in acetic acid with sodium nitrite; in addition, 4-phenyl-3-furoxanmethanol was obtained in 40% yield.
Synthesis of lathyrane diterpenoid nitrogen-containing heterocyclic derivatives and evaluation of their anti-inflammatory activities
Wang, Wang,Xiong, Liangliang,Li, Yutong,Song, Zhuorui,Sun, Dejuan,Li, Hua,Chen, Lixia
, (2022/01/24)
As our ongoing work on lathyrane diterpenoid derivatization, three series of lathyrane diterpenoid derivatives were designed and synthesized based combination principles, including pyrazole, thiazole and furoxan moieties. Biological evaluation indicated t
Synthesis and biological evaluation of NO-donor containing photosensitizers to induce ferroptosis of cancer cells
Guo, Xiuhan,Yu, Haoze,Shen, Wanjie,Cai, Rui,Li, Yueqing,Li, Guangzhe,Zhao, Weijie,Wang, Shisheng
, (2021/10/01)
Photodynamic therapy (PDT) is a non-invasive treatment method for tumors by exciting photosensitizers (PS) upon light irradiation to generate cytotoxic reactive oxygen species (ROS). However, the low oxygen concentration near the tumor tissue limits the t
Nitric oxide-releasing platinum(iv) prodrug efficiently inhibits proliferation and metastasis of cancer cells
Dai, Yi,Zhu, Yang,Cheng, Junjie,Shen, Juan,Huang, Hai,Liu, Manman,Chen, Zhaolin,Liu, Yangzhong
supporting information, p. 14051 - 14054 (2020/11/21)
A dual-functional Pt(iv) prodrug, Pt-furoxan, can release cytotoxic cisplatin and signaling molecule NO upon cellular internalization. NO modulates the cellular response towards cisplatin, leading to a synergistic anti-proliferation effect and a promising