The total synthesis of 14 membered macrolide Pestalotioprolide C and C7-epi- Pestalotioprolide C were accomplished starting from commercially available D-Mannitol by Stereoselective synthetic ...approach. The key reactions involved are Mitsunobu reaction, Regioselective ring opening of chiral epoxide and ring-closing metathesis reactions (RCM).
A new series of 1,3,4-oxadiazole bearing pyrimidine-pyrazine derivatives (9a-j) was developed and examined for their preliminary anticancer effects against four human cancer cell lines such as PC3 ...&DU-145 (prostate cancer), A549 (lung cancer) and MCF-7 (breast cancer). The well-known chemotherapeutic agent as etoposide used as a positive control. The IC
50
values range of target compounds from 0.05 ± 0.007 µM to 9.44 ± 5.36 µM, whereas positive control displayed values from 1.97 ± 0.45 µM to 3.08 ± 0.135 µM, respectively. Among them, five compounds (9a, 9b, 9c, 9g and 9j) exhibited most potent activities. Predominantly, one compound 9a showed superior activity.
A new library of tetrazole rings with oxazole-pyrimidine derivatives (9a-j) has been developed and synthesized. All of the compounds were characterized using spectral data. These were then tested for ...in vitro anticancer activity against four human cancer cell lines: prostate cancer (PC3 & DU-145), lung cancer (A549), and breast cancer (MCF-7) using an MTT assay. Etoposide was chosen as the positive control. Most of the compounds demonstrated moderate to good activity. These compounds (9a, 9b, 9d, 9g, and 9h) demonstrated the most powerful action. Particularly, one chemical 9h had exceptional antitumor efficacy.
A new series of amide derivatives (9a-j) have been synthesized and their chemical structures characterized by the
1
HNMR,
13
CNMR, and mass spectroscopic techniques. The synthesized amide derivatives ...(9a-j) were evaluated for their in vitro anti-proliferative activity against four human cancer cell lines, including PC3 (prostate cancer), A549 (lung cancer), MCF7 (breast cancer), and A2780 (ovarian cancer) cells by employing the MTT assay. Results were expressed as IC50 values and were compared with the clinical drug, etoposide, used as a positive control. Among the synthesized amide derivatives, five compounds 9a, 9b, 9c, 9d, and 9g revealed potent anti-proliferative potential toward all cell lines. Primarily, two compounds 9a and 9b possessed the most promising anticancer activities.
A new library of 1,3,4-thiadiazole bearing 1,3,5-triazine-thiazole (9a-j) compounds have been designed, synthesized, and assessed for their in vitro anticancer applications against a panel of human ...cancer cell lines, including prostate cancer (PC3&DU-145), lung cancer (A549), and breast cancer (MCF-7) by using the MTT method. The results were expressed as IC50 µM. Most of the tested compounds displayed good to moderate activity and were compared with the standard compound etoposide. The IC
50
values ranged for synthesized compounds from 0.11 ± 0.078 to 10.6 ± 5.47 µM and etoposide showed values ranging from 1.97 ± 0.45 to 3.08 ± 0.135 µM. Among the evaluated compounds, five (9a, 9b, 9c, 9d, and 9e) were found to show more potent activity. Specifically, compound 9a displayed good activity.
A new library of Aryl Benzimidazole-Pyridones (9a-j) has been synthesized, their structures were determined by
1
HNMR,
13
CNMR and mass spectral data. Further, these compounds explored for their ...anticancer application on four human cancer cell lines such as human prostate cancer cell line (PC3), lung cancer (A549), breast cancer (MCF-7) and human ovarian cancer (A2780) by employing MTT assay and results were compared with known anticancer agent asetoposide. All these compounds displayed remarkable cytotoxic activity. Among them, five compounds 9a, 9b, 9c, 9h and 9i displayed more potent activity. All compounds exhibited a discerning cytotoxic effect on cancer cells while not affecting normal Vero cells (IC50 = >22 µM), so providing justification for the strategic design approach employed in the development of a targeted anticancer drug.
A new library of 1,2,3-triazole linked isoflavone derivatives (9a-j) were synthesized and their structures were confirmed by
1
HNMR,
13
CNMR and mass spectral data. Further, the preliminary ...anticancer activities of compounds were evaluated against human prostate cancer (PC3 and DU-145), lung cancer (A549) and breast cancer (MCF-7) cell lines by using of MTT assay. Most of the tested compounds displayed good anticancer activity to compared with etoposide. Among the tested compounds, five compounds 9a, 9b, 9c, 9d and 9j possessed more potent activity than etoposide. In addition, Docking studies were also done on these compounds to probe the possible binding site interactions which corroborated well with the in vitro results.
A new bunch of substituted aryl amino derivatives structurally modified pyrido3,2-dpyrimidines (10a-j) have been synthesized and evaluated for anticancer effects against PC3 (human prostate), A549 ...(human lung), MCF-7 (human breast) and Colo-205 (human colon) cancer cell lines by utilizing of MTT procedure. Most of the synthesized compounds were showed anticancer activity good to moderate activities with IC
50
values range from 0.013 ± 0.0058 µM to 8.22 ± 5.87 µM, whereas, standard 9 etoposide used as standard drug) showed IC
50
values from 0.14 ± 0.017 µM to 3.08 ± 0.135 µM, respectively. Among the synthesized compounds, five compounds 10a, 10b, 10c, 10d and 10e demonstrated more potent activity on all cell lines. Mainly, compound 10e displayed higher anticancer activity.
In this article, a novel synthetic route was described for the total synthesis of Sporiolide B from inexpensive and commercially available starting materials by a concise fourteen-step sequence in ...6.50% overall yield. This convergent synthesis utilizes Grignard reaction, Asymmetric dihydroxylation, Yamaguchi macrolactonization and ring closing metathesis as the key steps.
An alternative total synthesis of Aigialomycin D D G S, Sudhakar; Ch, Venkata Ramana Reddy; Syed, Tasqeeruddin ...
Synthetic communications,
6/17/2024, Letnik:
54, Številka:
12
Journal Article
Recenzirano
Aigialomycin D, a 14-membered benzannulated macrolactone, was synthesized in a simple, efficient and stereoselective approach using inexpensive and commonly accessible starting materials. The main ...steps in this convergent synthesis are Corey-Fuchs reaction, Yamaguchi esterification and ring closing metathesis (RCM).
