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. 2022 Aug 15;27(16):5192. doi: 10.3390/molecules27165192

Table 2.

List of various potential synthetic HIF-1α inhibitors based on their mode of action in different cancers.

graphic file with name molecules-27-05192-i022.jpg

Serial
No.
Name Structure Mode of Action Effective against Cancer Type Clinical Trial Reference
1 YC-1 graphic file with name molecules-27-05192-i023.jpg HIF-1α synthesis blocker Hepatoma, gastric cancer, lung cancer, prostate cancer, pancreatic cancer, Human Bladder
Transitional Carcinoma
----- [127,133,195,196,197,198,199,200,201,202]
2 PX-478 graphic file with name molecules-27-05192-i024.jpg Colon carcinoma, Lung Adenocarcinoma, pancreatic ductal adenocarcinoma Phase I [127,133,203,204]
3 DJ12 graphic file with name molecules-27-05192-i025.jpg HIF-1α activity blocker Breast cancer, Melanoma, Renal cancer ----- [127,133,205]
4 Bortezomib graphic file with name molecules-27-05192-i026.jpg Human hepatoma, multiple myeloma, human embryonic kidney and human multiple myeloma Approved [127,133,206,207,208]
5 Amphotericin B (AmB) graphic file with name molecules-27-05192-i027.jpg Hepatocellular carcinoma, Approved [127,133,209]
6 Polyamides graphic file with name molecules-27-05192-i028.jpg Adenocarcinoma ----- [127,133,210]
7 ENMD-1198 (Analog of 2ME2) graphic file with name molecules-27-05192-i029.jpg HIF-1α degradation enhancer Prostate cancer, breast cancer, human hepatocellular carcinoma ----- [127,133,211,212,213]
8 Zebularine
graphic file with name molecules-27-05192-i030.jpg Oral squamous cell carcinoma ----- [127,133,214]
9 17-AAG (Analog of Geldanamycin)
graphic file with name molecules-27-05192-i031.jpg Prostate cancer, renal cell carcinoma, papillary thyroid carcinoma Phase III [127,133,215,216]
10 Flavopiridol graphic file with name molecules-27-05192-i032.jpg Leukemia, human glioma, neuroblastoma Phase II [127,133,217,218,219,220,221,222]