Indoline ureas as potential anti-hepatocellular carcinoma agents targeting VEGFR-2: Synthesis, in vitro biological evaluation and molecular docking

Saffron-Based Crocin Prevents Early Lesions of Liver Cancer: In vivo, In vitro and Network Analyses

“…Sorafenib has been reported beneficial at early stages of HCC, yet its effectiveness as an angiogenesis inhibitor has been modest [6]. As vascular endothelial growth factor (VEGF) is highly expressed in HCC liver [7,8], Phase III study is currently underway to evaluate the effect of regorafenib, a derivative of sorafenib that inhibits angiogenic kinases like VEGFR-1/3 and its efficacy and safety in HCC patients [9]. VEGF receptors-3 has been shown to be differentially upregulated on tumor vasculature supporting the majority of solid cancers including HCC.…”

Synthesis and biological evaluation of certain hydrazonoindolin-2-one derivatives as new potent anti-proliferative agents

“…It is a multikinase inhibitor that targets VEGFR-1, VEGFR-2, PDGFRb, and c-Kit. Recently, our research group has paid much attention to develop many novel small molecules based on the indolin-2-one core as potent anticancer agents [14][15][16][17][18][19][20][21][22] . In 2017, we reported two studies 14,15 regarding development of hydrazonoindolin-2-onebased derivatives and evaluation of their anti-proliferative activity against A549 (lung), HT-29 (colon), and ZR-75 (breast) human cancer cell lines, beside evaluation of their pro-apoptotic activity.…”

“…Based on the aforementioned findings and in connection with our research program on the development of indolin-2-one-based anticancer candidates [14][15][16][17][18][19][20][21][22] , it was thought worthwhile to extend our investigations to probe certain hydrazonoindolin-2-ones displaying promising anti-proliferative activity. In this study, we reported the design and synthesis of different series of hydrazonoindolin-2-ones 3a-e, 5a-e, 7a-c, and 10a-l, adopting three distinctive strategies to develop such derivatives (Figure 2).…”

<em>p</em>-TSA-promoted syntheses of 5H-benzo[h]thiazolo[2,3-b]quinazoline and indeno[1,2-d]thiazolo[3,2-a]pyrimidine analogs: molecular modeling and in vitro antitumor activity against hepatocellular carcinoma

“…The most prevalent primary liver cancer with poor prognosis is hepatocellular carcinoma (HCC), which has potentially lethal human malignacy worldwide, particularly in Asia and Africa 1,2. In men, HCC is the fifth most commonly diagnosed cancer and the second leading cause of cancer deaths; in women, it is the seventh most frequently diagnosed cancer, and worldwide, overall, it is the sixth commonest cause of cancer-related deaths 3. In spite of continuous efforts to develop novel therapeutic strategies to treat HCC, it remains a challenge.…”