Benzothiazole-Phthalimide Hybrids as Anti-Breast Cancer and Antimicrobial Agents
Abstract
:1. Introduction
2. Results
2.1. Chemistry
2.2. Biological Results
2.2.1. Cell Viability Assay
2.2.2. Antibacterial Studies
2.2.3. Antifungal Studies
2.2.4. Compound 3h Induces DNA Damage in MDA-MB-231 Cells
2.2.5. Effect of Compound 3h on Cell Migration
2.2.6. ROS Scavenging Effect of Compound 3h
3. Discussion
4. Materials and Methods
4.1. Chemistry
4.2. Biology
4.2.1. Cell Culture
4.2.2. Cell Viability
4.2.3. Antibacterial Studies
4.2.4. Antifungal Studies
4.2.5. TUNEL Assay
4.2.6. Wound-Healing Assay
4.2.7. ROS Protection Assay
5. Conclusions
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
References
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Compounds | MW a | MP b (°C) | LogS c | LogP d |
---|---|---|---|---|
3a | 280.30 | 249–250 | –4.81 | 3.04 |
3b | 298.29 | 234–235 | –5.09 | 3.18 |
3c | 348.30 | > 250 | –5.82 | 3.93 |
3d | 294.33 | > 250 | –5.32 | 3.51 |
3e | 310.33 | 227–229 | –4.82 | 2.79 |
3f | 340.35 | > 250 | –4.78 | 2.54 |
3g | 296.30 | > 250 | –4.39 | 2.76 |
3h | 372.40 | > 250 | –6.67 | 4.47 |
Compounds | MDA-MB-231 | MCF-7 | MCF10-A |
---|---|---|---|
3a | 81.8 ± 0.8 | 165.5 ± 1.1 | >500 |
3b | 71.2 ± 1.0 | 91.5 ± 0.6 | 151.9 ± 1.1 |
3c | >500 | >500 | >500 |
3d | 202.6 ± 0.6 | 66.0 ± 1.2 | >500 |
3e | 102.8 ± 0.9 | 223.1 ± 0.9 | >500 |
3f | 49.6 ± 1.0 | 93.0 ± 1.4 | >500 |
3g | 63.3 ± 0.7 | 71.2 ± 0.7 | >500 |
3h | 14.0 ± 0.5 | 26.2 ± 0.9 | 193.9 ± 1.0 |
thalidomide | 413.0 ± 2.0 | 360.0 ± 2.0 | >500 |
Microorganisms | ||||||||
---|---|---|---|---|---|---|---|---|
Gram-Positive | Gram-Negative | |||||||
S.a. 25923 | S.a. 29213 | S.a. 43300 | E.f. 29212 | A.b. 19606 | E.c. 25922 | K.p. 13883 | P.a. 27853 | |
3a | 64 | 64 | 64 | 64 | 64 | 64 | 128 | 64 |
3b | 64 | 64 | 64 | 64 | 128 | 64 | 128 | 64 |
3c | 128 | 128 | 64 | 64 | 128 | 128 | 128 | 128 |
3d | >512 | >512 | >512 | >512 | >512 | >512 | >512 | >512 |
3e | 32 | 64 | 32 | 64 | 64 | 64 | 64 | 64 |
3f | 32 | 64 | 32 | 32 | 64 | 32 | 64 | 64 |
3g | 32 | 64 | 32 | 32 | 64 | 64 | 64 | 64 |
3h | 16 | 32 | 32 | 32 | 32 | 32 | 32 | 32 |
levofloxacin | 0.5 | 0.5 | 0.5 | 2 | 8 | 0.06 | 8 | 4 |
Microorganisms | ||||
---|---|---|---|---|
C.a. 10231 | C.a. 90028 | C.g. 15126 | C.p. 22019 | |
3a | 64 | 64 | 32 | 32 |
3b | 64 | 64 | 32 | 32 |
3c | 64 | 64 | 64 | 64 |
3d | >512 | >512 | >512 | >512 |
3e | 64 | 64 | 64 | 32 |
3f | 32 | 64 | 32 | 32 |
3g | 32 | 64 | 32 | 32 |
3h | 32 | 32 | 16 | 16 |
amph B | 2 | 1 | 2 | 2 |
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Barbarossa, A.; Ceramella, J.; Carocci, A.; Iacopetta, D.; Rosato, A.; Limongelli, F.; Carrieri, A.; Bonofiglio, D.; Sinicropi, M.S. Benzothiazole-Phthalimide Hybrids as Anti-Breast Cancer and Antimicrobial Agents. Antibiotics 2023, 12, 1651. https://doi.org/10.3390/antibiotics12121651
Barbarossa A, Ceramella J, Carocci A, Iacopetta D, Rosato A, Limongelli F, Carrieri A, Bonofiglio D, Sinicropi MS. Benzothiazole-Phthalimide Hybrids as Anti-Breast Cancer and Antimicrobial Agents. Antibiotics. 2023; 12(12):1651. https://doi.org/10.3390/antibiotics12121651
Chicago/Turabian StyleBarbarossa, Alexia, Jessica Ceramella, Alessia Carocci, Domenico Iacopetta, Antonio Rosato, Francesco Limongelli, Antonio Carrieri, Daniela Bonofiglio, and Maria Stefania Sinicropi. 2023. "Benzothiazole-Phthalimide Hybrids as Anti-Breast Cancer and Antimicrobial Agents" Antibiotics 12, no. 12: 1651. https://doi.org/10.3390/antibiotics12121651