Steering the antitumor drug discovery campaign towards structurally diverse indolines
Amandeep Thakur, Arshdeep Singh, Navdeep Kaur, Ritu Ojha, Kunal Nepali
TMU Biomedical Commercialization Center
Indoline framework is often perpended as a privileged heterocycle present in medicinally valuable compounds of natural and synthetic origin. This review article presents the rational approaches/strategies employed for the design of anticancer indolines along with the structure activity relationship and mechanistic insights revealed in the in-vitro and in-vivo assays. The chemist has always been fascinated towards the indoline ring for the construction of antitumor scaffolds owing to its versatility as evidenced by its existence in scaffolds inducing antiproliferative effects via diverse mechanisms. To the delight of medicinal chemist, the applicability of indoline has also been expanded towards the design of dual inhibitors (multitargeting anticancer agents) as well as PROTACS. Overall, it can be concluded that indoline moiety is a magic bullet and the scaffolds containing this ring are foraying towards detailed preclinical and clinical stage investigations by leaps and bounds.
Bioorganic Chemistry
https://doi.org/10.1016/j.bioorg.2019.103436
Dearomatization
Indolines
Thakur, A., Singh, A., Kaur, N., Ojha, R., & Nepali, K. (2020). Steering the antitumor drug discovery campaign towards structurally diverse indolines. Bioorganic Chemistry, 94, [103436]. https://doi.org/10.1016/j.bioorg.2019.103436
Steering the antitumor drug discovery campaign towards structurally diverse indolines. / Thakur, Amandeep; Singh, Arshdeep; Kaur, Navdeep; Ojha, Ritu; Nepali, Kunal.
In: Bioorganic Chemistry, Vol. 94, 103436, 01.2020.
Thakur, A, Singh, A, Kaur, N, Ojha, R & Nepali, K 2020, 'Steering the antitumor drug discovery campaign towards structurally diverse indolines', Bioorganic Chemistry, vol. 94, 103436. https://doi.org/10.1016/j.bioorg.2019.103436
Thakur A, Singh A, Kaur N, Ojha R, Nepali K. Steering the antitumor drug discovery campaign towards structurally diverse indolines. Bioorganic Chemistry. 2020 Jan;94. 103436. https://doi.org/10.1016/j.bioorg.2019.103436
Thakur, Amandeep ; Singh, Arshdeep ; Kaur, Navdeep ; Ojha, Ritu ; Nepali, Kunal. / Steering the antitumor drug discovery campaign towards structurally diverse indolines. In: Bioorganic Chemistry. 2020 ; Vol. 94.
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title = "Steering the antitumor drug discovery campaign towards structurally diverse indolines",
abstract = "Indoline framework is often perpended as a privileged heterocycle present in medicinally valuable compounds of natural and synthetic origin. This review article presents the rational approaches/strategies employed for the design of anticancer indolines along with the structure activity relationship and mechanistic insights revealed in the in-vitro and in-vivo assays. The chemist has always been fascinated towards the indoline ring for the construction of antitumor scaffolds owing to its versatility as evidenced by its existence in scaffolds inducing antiproliferative effects via diverse mechanisms. To the delight of medicinal chemist, the applicability of indoline has also been expanded towards the design of dual inhibitors (multitargeting anticancer agents) as well as PROTACS. Overall, it can be concluded that indoline moiety is a magic bullet and the scaffolds containing this ring are foraying towards detailed preclinical and clinical stage investigations by leaps and bounds.",
keywords = "Alkaloids, Cancer, Cells, Dearomatization, Heterocycles, Indolines, Tumor",
author = "Amandeep Thakur and Arshdeep Singh and Navdeep Kaur and Ritu Ojha and Kunal Nepali",
doi = "10.1016/j.bioorg.2019.103436",
journal = "Bioorganic Chemistry",
T1 - Steering the antitumor drug discovery campaign towards structurally diverse indolines
AU - Thakur, Amandeep
AU - Singh, Arshdeep
AU - Kaur, Navdeep
AU - Ojha, Ritu
AU - Nepali, Kunal
N2 - Indoline framework is often perpended as a privileged heterocycle present in medicinally valuable compounds of natural and synthetic origin. This review article presents the rational approaches/strategies employed for the design of anticancer indolines along with the structure activity relationship and mechanistic insights revealed in the in-vitro and in-vivo assays. The chemist has always been fascinated towards the indoline ring for the construction of antitumor scaffolds owing to its versatility as evidenced by its existence in scaffolds inducing antiproliferative effects via diverse mechanisms. To the delight of medicinal chemist, the applicability of indoline has also been expanded towards the design of dual inhibitors (multitargeting anticancer agents) as well as PROTACS. Overall, it can be concluded that indoline moiety is a magic bullet and the scaffolds containing this ring are foraying towards detailed preclinical and clinical stage investigations by leaps and bounds.
AB - Indoline framework is often perpended as a privileged heterocycle present in medicinally valuable compounds of natural and synthetic origin. This review article presents the rational approaches/strategies employed for the design of anticancer indolines along with the structure activity relationship and mechanistic insights revealed in the in-vitro and in-vivo assays. The chemist has always been fascinated towards the indoline ring for the construction of antitumor scaffolds owing to its versatility as evidenced by its existence in scaffolds inducing antiproliferative effects via diverse mechanisms. To the delight of medicinal chemist, the applicability of indoline has also been expanded towards the design of dual inhibitors (multitargeting anticancer agents) as well as PROTACS. Overall, it can be concluded that indoline moiety is a magic bullet and the scaffolds containing this ring are foraying towards detailed preclinical and clinical stage investigations by leaps and bounds.
KW - Alkaloids
KW - Cells
KW - Dearomatization
KW - Heterocycles
KW - Indolines
KW - Tumor
U2 - 10.1016/j.bioorg.2019.103436
DO - 10.1016/j.bioorg.2019.103436
JO - Bioorganic Chemistry
JF - Bioorganic Chemistry
10.1016/j.bioorg.2019.103436